Panobinostat
Panobinostat, sold under the brand name Farydak, is a medication for the treatment of various cancers. It is, in fact, a hydroxamic and acts as a non-selective histone deacetylase inhibitor. Experts use Panobinostat in combination with bortezomib (Velcade) and also dexamethasone to treat people with multiple myeloma (a type of cancer of the bone marrow) who have already been got a treatment with two other medications, including bortezomib (Velcade). Panobinostat is in fact, in a class of medications called histone deacetylase (HDAC) inhibitors. However, it works by killing cancer cells.
On 23 February 2015 it received FDA accelerated approval for use in patients with multiple myeloma; and on 28 August 2015, the European Medicines Agency approved it for the same use. As of August 2012, it is being tested against Hodgkin’s lymphoma, cutaneous T cell lymphoma (CTCL) and other types of malignant disease in Phase III clinical trials, against myelodysplastic syndromes, breast cancer and prostate cancer in Phase II trials, and against chronic myelomonocytic leukaemia (CMML) in a Phase I trial.
Moreover, as of 2014 panobinostat is in use in a Phase I/II clinical trial that aims at curing AIDS in patients on highly active antiretroviral therapy (HAART). In this technique, experts use panobinostat to drive the HIV DNA out of the patient’s DNA, in the expectation that the patient’s immune system in combination with HAART will destroy it. As of 2016 panobinostat is being studied in a phase II trial for relapsed and refractory diffuse large B-cell lymphoma (DLBCL)
Panobinostat inhibits multiple histone deacetylase enzymes, a mechanism leading to apoptosis of malignant cells via multiple pathways. Panobinostat is absorbed quickly and almost completely from the gut, but has a significant first-pass effect, resulting in a total bioavailability of 21%. The highest blood plasma levels in patients with advanced cancer are reached after two hours. Plasma protein binding is about 90%. The substance is metabolised mainly through oxidation by the liver enzyme CYP3A4 and to a small extent by CYP2D6 and CYP2C19. It is also reduced, hydrolyzed and glucuronidized by unspecified enzymes. All metabolites seem to be inactive. The biological half-life is approximately 37 hours, as per the estimates. The urine excretes 29–51%, while the faeces 44–77%.
Panobinostat comes as a capsule to take by mouth. People usually take it with or without food once daily on certain days of a 21-day cycle. Also, one may repeat the cycle for up to 16 cycles. Take panobinostat at around the same time on each scheduled day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take panobinostat exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Swallow the capsules whole with a glass of water; do not crush, chew, or open them. Handle the capsules as little as possible. If you touch a broken panobinostat capsule or the medicine in the capsule, wash that area of your body with soap and water. In case the medicine in the capsule gets into your mouth, nose, or eyes, wash it away with plenty of water. If you vomit after taking panobinostat, do not take another dose. Continue your regular dosing schedule.
Be sure to tell your doctor how you are feeling during your treatment. Your doctor may decrease your dose of panobinostat or stop your treatment for a while or permanently if you experience side effects of the medication.
Side effects:
- weight loss
- Headache
- black, tarry, or bloody stools
- bloody vomit or vomited material that looks like coffee grounds
- unusual bruising or bleeding
- pink or brown urine
- blood in phlegm
- confusion
- changes in your speech
- fever, cough, chills, sweating or other signs of infection
- pale skin
- nausea, vomiting, loss of appetite, dark urine, stomach pain, extreme tiredness, lack of energy, or yellowing of skin or white of eyes
Symptoms of overdose may include the following:
- diarrhoea
- nausea
- vomiting
- decreased appetite
